Drug intelligence / Profile preview

mirtazapine + bupivacaine + morphine

Development stage
Unknown
Lead developer
Organon
Modality
Small Molecules
Administration
Oral, Intravenous, Intrathecal, Epidural
01

Overview

This is a combination of three drugs—mirtazapine, bupivacaine, and morphine—used together primarily in the context of perioperative or postoperative pain management. - **Mirtazapine** is a tetracyclic antidepressant that acts as an antagonist at central presynaptic alpha-2 adrenergic inhibitory autoreceptors and heteroreceptors, increasing noradrenergic and serotonergic activity. It also blocks 5-HT2 and 5-HT3 serotonin receptors, which may contribute to its antipruritic effects when used with neuraxial opioids[3][4][7]. - **Bupivacaine** is a long-acting local anesthetic that blocks voltage-gated sodium channels in neuronal membranes, inhibiting nerve impulse conduction to provide regional anesthesia[4][5]. - **Morphine** is an opioid analgesic that acts primarily as an agonist at the mu-opioid receptor in the central nervous system to produce analgesia. When administered intrathecally or epidurally with local anesthetics like bupivacaine, it provides prolonged pain relief but can cause side effects such as pruritus[4][5]. The combination of these agents leverages their complementary mechanisms for enhanced postoperative analgesia while potentially reducing opioid-induced side effects such as pruritus through mirtazapine’s serotonergic antagonism[1][7].

02

Targets

ADRA2 (Adrenergic alpha-2 receptor family)HRH1 (Histamine H1 Receptor)HTR2A (5-hydroxytryptamine receptor 2A)HTR2C (5-hydroxytryptamine 2C receptor)HTR3A (5-hydroxytryptamine receptor 3A)MOR (Mu opioid receptor)SCN5A (Sodium channel protein type 5 subunit alpha)ADRA2A (α2A)5-HT2 (5-HT2 receptor family)NaV (Voltage-gated sodium channels)

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